Abstract
A series of substituted 2-aminobenzothiazole compounds have been synthesized and evaluated as nitric oxide synthase (NOS) inhibitors. Compound 14 shows activity in the nM range and is selective for the human neuronal NOS isoform. We have also evaluated the compounds against the rat NOS isoforms. For some of the compounds, there are significant differences in NOS inhibitory activities between the human and rat enzymes. For example, compound 10b has nM activity against the rat nNOS while low microM activity against the human nNOS.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzothiazoles / chemistry*
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Benzothiazoles / pharmacology
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Humans
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Inhibitory Concentration 50
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Isoenzymes
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Models, Chemical
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Molecular Conformation
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Nitric Oxide Synthase Type I / antagonists & inhibitors*
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Rats
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Thiazoles / chemical synthesis*
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Thiazoles / pharmacology
Substances
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Benzothiazoles
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Enzyme Inhibitors
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Isoenzymes
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Thiazoles
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Nitric Oxide Synthase Type I